Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Combination cancer therapy

A cancer and composition technology, applied in the field of conjugates of cytarabine and aspartic acid, can solve the problem of high toxicity of cytarabine

Pending Publication Date: 2020-03-06
BIOSIGHT
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cytarabine is highly toxic with severe side effects such as cerebellar toxicity and myelosuppression

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Combination cancer therapy
  • Combination cancer therapy
  • Combination cancer therapy

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0413] Effects of Asp-cytarabine / BST-236 and azacitidine (Vidaza) on the proliferation and survival of U937 cells

[0414] U937 human blood cancer cells were cultured in RPMI supplemented with 10% FCS. cells at 1x10 5 Cells / well were seeded in a 96-well plate in a total volume of 250 μl. Azacitidine (AZA) was added to the cell culture at 5 different concentrations: 0, 100, 250, 1000, 5000 nM. Asp-cytarabine, hereafter also referred to as BST-236, was added to the cultures at a concentration of 250 nM. All groups were analyzed in triplicate. at 37°C with 5% CO 2 After 72 hours of incubation at 0°C, cells were harvested, stained with propidium iodide (PI), and immediately read by FACS. The number and percentage of live (PI-negative) cells and the number and percentage of dead (PI-positive) cells in the cultures were determined by FACScalibur using CellQuest software. Calculate percent inhibition.

[0415] Table 2. Percent growth inhibition of U937 cells treated with Asp-c...

example 2

[0422] Effects of Asp-cytarabine and azacitidine on the proliferation of Molt-4 cells

[0423] The Molt-4 human leukemia cell line was obtained from ATCC. Cells were grown in RPMI medium containing 10% FBS and 1% glutamine. Cells were seeded in 96-well plates at 50,000 cells / ml, 0.2ml / well. Test substances were diluted in PBS and added at final concentrations of 0.1 nM to 10 μM in a volume of 20 μl. The study was performed in triplicate. PBS was used as a control. Incubate the plate at 37 °C with 5% CO 2 Incubate for 72 hours. At the end of the treatment period, an MTT assay using the MTT reagent [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] was performed. MTT was added to each well at a concentration of 5 mg / ml in a volume of 0.02 ml. Plates were incubated at 37°C for 3 hours. The plate was centrifuged at 3500 rpm for 5 minutes and the supernatant was aspirated. The pellets containing MTT crystals were each dissolved in 0.2 ml DMSO. Absorbance was m...

example 3

[0432] Effects of Asp-cytarabine and ABT-199 (venetoclax) on the proliferation and survival of U937 cells

[0433] U937 cells were cultured in RPMI supplemented with 10% FCS, and 1x10 5 Cells / well were seeded in a 96-well plate in a total volume of 250 μl. ABT-199 was added to cell cultures at 3 different concentrations: 0, 250 and 1000 nM. Asp-cytarabine was added to the cultures at a concentration of 250 nM. All groups were analyzed in triplicate. at 37°C with 5% CO 2 After 24 hours of incubation at 0°C, cells were harvested and stained with propidium iodide (PI) and read immediately by FACS. The number and percentage of live (PI-negative) cells and the number and percentage of dead (PI-positive) cells in the cultures were determined by FACScalibur using CellQuest software. Calculate percent inhibition.

[0434] Such as image 3 As shown in , treatment of human hematological cancer cells with the combination of Asp-cytarabine and ABT-199 for 24 hours resulted in a sig...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention relates to combination therapies of a cytarabine conjugate and one or more anti-neoplastic agents for inhibiting cancer cell growth. In particular, the present invention relatesto a conjugate of cytarabine and aspartic acid (BST-236) in combination with one or more additional anti-neoplastic agents for use in the treatment of hematological cancers.

Description

[0001] related application [0002] This patent application claims priority to US Provisional Application No. 62 / 530,213, filed July 9, 2017, which is hereby incorporated by reference in its entirety for all purposes. technical field [0003] The present invention relates to combination therapy of cytarabine conjugates and one or more additional antineoplastic agents for inhibiting the growth of cancer cells. In particular, the present invention relates to conjugates of cytarabine and aspartic acid for use in the treatment of hematological cancers in combination with one or more additional antineoplastic agents. Background technique [0004] antineoplastic agent [0005] Antineoplastic agents, also known as antiproliferative agents, antimetabolites, or covalent DNA-binding agents, act by inhibiting essential metabolic pathways and are commonly used to treat malignant diseases. However, their high toxicity to normal cells and severe side effects limit their use as therap...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7064A61K47/50A61P35/00C07H19/067
CPCC07H19/09A61P35/00A61K47/542A61K45/06A61K31/44A61K31/444A61K31/4709A61K31/506A61K31/53A61K31/5377A61K31/553A61K31/635A61K31/704A61K31/706A61K31/7068A61K31/7072A61K31/708A61K31/454A61K31/497A61P35/02A61K2300/00A61K31/496A61K31/4412A61K39/3955A61K9/0019A61K31/439A61K31/4965A61K31/7084
Inventor 鲁思·本亚喀尔斯泰拉·甘格里诺维奇所司·特斯勒利亚特·弗莱肖恩
Owner BIOSIGHT
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com